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UMI-77
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UMI-77图片
CAS NO:518303-20-3
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)468.34
FormulaC18H14BrNO5S2
CAS No.518303-20-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 93 mg/mL (198.6 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: Not available
Solubility (In vivo)5% DMSO+30% PEG 300+dd H2O: 6 mg/mL
实验参考方法
GeneralIn a BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg i.v.) exhibits single-agent antitumor activity without any damage normal tissues
Animal modelFemale BALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells.
FormulationObatoclax (tartrate salt) is formulated in 9.6% PEG300, 0.4% polysorbate 20, and 5% dextrose; while for the 4T1 tumor model, Obatoclax is formulated in 9.48% PEG, 0.38% polysorbate 20.
Dosages0.0313, 0.25, 0.5 and 2 mg/kg
AdministrationIntravenously (tail vein) once a day
References[1] Abulwerdi F, et al. Mol Cancer Ther. 2014, 13(3), 565-575.
生物活性

UMI77 disrupts the Mcl-1/Bak complex. Panc-1 (A) and BxPC-3 (B) cells were treated with the indicated concentrations of UMI77 for 48 hours and then prepared for immunoprecipitation and immunoblotting. Mcl-1 was immunoprecipitated from cell lysates and the levels of Bak interacting with Mcl-1 were detected by immunoblotting for Bak. Translational oncology 8(1):47-54, 2015

Downregulation of Mcl-1 by siRNA in BxPC-3 cells blocks growth inhibition and apoptosis induced by 2 (UMI-77). Mol Cancer Ther. 2014 Mar;13(3):565-75

Inhibition of Mcl-1 by UMI77 does not radiosensitize normal cells. CCL-241 normal small intestinal cells were treated with UMI77 (1-3μM) as illustrated (Figure 3A) and radiosensitization was assessed by clonogenic survival. Translational oncology 8(1):47-54, 2015